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At least 163 records · Page 9Linked to original sources
PubMed1991

High-performance liquid chromatography post-column derivatization with fluorescence detection to study the influence of ambroxol on dipalmitoylphosphatidylcholine levels in rabbit eustachian tube washings.

In this work an appropriate high-performance liquid chromatography method was set up to guarantee specificity, sensitivity, precision and accuracy in analyzing dipalmitoylphosphatidylcholine (DPPC) in rabbit eustachian tube washings, as well as to determine its varying levels after administration of ambroxol chloride. The procedure is based on a post-column derivatization with fluorescence detection using 1,6-diphenyl-1,3,5-hexatriene which exhibits increased fluorescence in a lipid environment. DPPC was chromatographed on a Hypersil C18. The mobile phase for the isocratic elution consisted of 40 mmol/l choline chloride in methanol-tetrahydrofuran (97:3). Ambroxol was given to a group of New Zealand white rabbits at a dose of 30 mg/kg. A second group receiving vehicle only acted as controls.

1,2-Dipalmitoylphosphatidylcholine↗
PubMed2000

Sensitive method for the determination of ambroxol in body fluids by capillary electrophoresis and fluorescence detection.

A sensitive and rapid capillary electrophoretic method combined with laser-induced fluorescence detection has been developed for the determination of ambroxol. Samples were derivatized with 5 x 10(-4) M fluorescein isothiocyanate. A linear relationship between concentration and peak area was obtained in the concentration range 0.008-42 microg ml(-1) with a correlation coefficient of 0.9999. The applicability of the method to serum and urine samples was demonstrated. The method is also useful for the determination of ambroxol in pharmaceutical preparations.

Ambroxol↗
PubMed2003

Quantitative determination of ambroxol in tablets by derivative UV spectrophotometric method and HPLC.

A derivative UV spectrophotometric method for the determination of ambroxol in tablets was developed. Determination of ambroxol in tablets was conducted by using first-order derivative UV spectrophotometric method at 255 nm (n = 5). Standards for the calibration graph ranging from 5.0 to 35.0 microg/ml were prepared from stock solution. The proposed method was accurate with 98.6+/-0.4% recovery value and precise with coefficient of variation (CV) of 1.22. These results were compared with those obtained by reference methods, zero-order UV spectrophotometric method and reversed-phase high-performance liquid chromatography (HPLC) method. A reversed-phase C(18) column with aqueous phosphate (0.01 M)-acetonitrile-glacial acetic acid (59:40:1, v/v/v) (pH 3.12) mobile phase was used and UV detector was set to 252 nm. Calibration solutions used in HPLC were ranging from 5.0 to 20.0 microg/ml. Results obtained by derivative UV spectrophotometric method was comparable to those obtained by reference methods, zero-order UV spectrophotometric method and HPLC, as far as ANOVA test, F(calculated) = 0.762 and F(theoretical) = 3.89, was concerned.

Ambroxol↗
PubMed1987

Ambroxol increases the choline but not fatty acid incorporation into lung phospholipids in experimental lung disorders.

Ambroxol, a drug capable of elevating the phospholipid content in healthy rabbit lungs, was tested on two models of experimental lung injury, lung changes in sepsis induced by a peritonitis and in bromcarbamide intoxication. The phospholipid content of the lungs and the synthesis of the individual phospholipids phosphatidylcholine (PC) and sphingomyeline were measured in vitro by incubation of lung slices with labeled phospholipid precursors. Influenced by the drug, the phospholipid content increases to 132% in the peritonitis experiments and to 111% in the bromcarbamide experiments. The peritonitis experiments show the increase in phospholipid synthesis to result from an enhanced choline incorporation into PC up to 192% and into sphingomyeline up to 630%. The values for the bromcarbamide experiments are 411% for PC and 485% for sphingomyeline, respectively. There was no statistically significant difference in the incorporation of fatty acids in the treated and untreated animals. We conclude that ambroxol possibly stimulates the phospholipid synthesis in injured lungs by stimulating the choline phosphatcytidyltransferase, but not the incorporation of fatty acids into PC in those lungs. These findings may be important to the surfactant system of the lung consisting mainly of PC.

Ambroxol↗
PubMed2005

Determination of ambroxol in an automated multi-pumping pulsed flow system.

A new flow methodology exploiting the multi-pumping approach was developed for the spectrophotometric determination of ambroxol hydrochloride in pharmaceutical preparations. The flow manifold was implemented by using, exclusively, multiple solenoid-actuated micro-pumps, which acted simultaneously as sample insertion, solutions propelling and reagents commutation units. Linear calibration plots were obtained over an ambroxol concentration ranging from 10 to 200 mg l(-1) (r.s.d. < 0.5%, n = 15) and a sampling rate of about 60 samples per hour (flow rate = 1.92 ml min(-1), sample volume = 80 microl).

Ambroxol↗
PubMed2004

[A near-infrared diffuse reflectance analysis method for the noninvasive quantitative analysis of ambroxol hydrochloride tablets].

AIM: To develop a near-infrared diffuse reflectance analysis (NIRDRA) method for rapid noninvasive quantitative determination of ambroxol hydrochloride in half-finished product particles and non-blister-packed, blistered tablets. METHODS: All spectra were measured with a Fourier transform spectrometer equipped with a PbS and a InGaAs detector, an external integrating sphere, a rotating sample cup, and a fibre-optic probe for reflectance measurements. All samples were scanned from 12,000 cm-1 to 4,000 cm-1, and each sample spectrum was obtained as an automatic mean of 64 scans. No spectrum pre-processing method was used, and spectral regions, 4,602-4,247, 12,000-7,498 and 6,102-5,446, 12,000-5,446 cm-1 were selected to develope mathematical models by partial least square method for half-finished product particles and non-blister-packed, blistered tablets samples, respectively. RESULTS: The optimal rank and mean square error determined for half-finished product particles and non-blister-packed, blistered tablets samples by cross validation method all was 6 and 0.306, 0.972 and 1.492, respectively, the average recovery was 100%, 100% and 102% respectively; and the RSD was 1.17%, 1.70% and 1.78% respectively. CONCLUSION: Results showed that the NIRDRA method was rapid, simple, noninvasive and sensitive, and it can be applied to assay the content of ambroxol hydrochloride in half-finished product particles non-blister-packed and blistered tablets.

Ambroxol↗
PubMedDate not supplied

The influence of ambroxol and capsaicin on the isolated rabbit bladder wall.

Unmyelinated C-fibers endings lye beneath the epithelial layer and release neuropeptides which regulate baseline transepithelial potential difference (PD) and changes of transepithelial potential difference during mechanical stimulation (dPD). Ambroxol can suppress reflexes such as the cough or the corneal reflex which are connected to stimulation of C fibre endings. The study aimed to estimate the influence of ambroxol (ABX) and capsaicin (CAPSA) on PD and dPD in isolated rabbit bladder. The experiments were carried out on 26 bladder specimens of. 2 cm2 surface area each, obtained from 13 rabbits. Ussing apparatus was used. Procedure used for stimulation of sensory receptor involved directing stream onto epithelium. A stimulus lasted 30s, ejecting the 2.5 ml fluid. Amiloride and bumetanide were used to estimate of ionic currents. Each significant reaction was repeated at least 10 times on various specimens. PD ranged between 5 and 10 mV in different experimental conditions. Mechanical stimulation of isolated bladder wall caused increasing dPD about 2 mV defined as hyperpolarization. Application of ABX to the stimulation fluid decreased the hyperpolarization in comparison with control stimulation under conditions of inhibited chloride ion transport. Application of CAPSA to the stimulation fluid decreased the hyperpolarization in comparison with control stimulation under conditions of inhibited sodium ion transport. ABX and CAPSA had no influence on PD after mechanical stimulation. ABX as well as CAPSA influence on transepithelial ion transport pathways in bladder epithelium is dependent on sensory stimulation. ABX can be suspected to suppress bladder contractions.

Ambroxol↗
PubMed1986

[The effect of ambroxol and bromhexine on the "respiratory burst" of alveolar macrophages].

The effect of ambroxol and bromhexine on the yeast cell wall- and arachidonic acid (AA)-induced luminol-respectively lucigenin-dependent chemiluminescence (CL) of alveolar macrophages (AM) of patients with lung diseases has been investigated. Both drugs cause a suppression of the induced CL. These results suggest that ambroxol and bromhexine reduce the generation of reactive oxygen metabolites (ROM) by AM. The mechanism of action is thought to involve the activation of the acyl-CoA: lysophosphatide acyltransferase. The increase of this enzyme activity lowers probably the intracellular concentration of free AA and consequently also the production of ROM. The investigations show a new possibility for the influence of biosynthesis of ROM and likely of eicosanoids, which play an important role as pathogenetic mediators in different lung diseases.

Acridines↗
PubMed1987

The pharmacology of ambroxol--review and new results.

The major pharmacodynamic actions of ambroxol are surfactant stimulation, mucokinetic and secretagogue activity. The therapeutic activities of the drug in animal models of the infant and adult respiratory distress syndrome (IRDS and ARDS) are reviewed. SO2 exposed rats, which exhibited increased airway resistance and work of breathing, were used as an animal model of a bronchitic syndrome. The active group was treated with 25 mg kg-1 oral ambroxol for 10 days. The airway resistance of this group (53.6 +/- 7.0 Pa.ml-1.s) was significantly lower than that of the control (81.2 +/- 11.4). Specific work of breathing was also lower in the treated group (0.26 +/- 0.02 mJ.ml-1, control: 0.35 +/- 0.029). The alleviation of airflow limitation was a consequence of subacute treatment and not of acute bronchodilatation. Treatment with the beta 2-adrenergic drug clenbuterol further improved both active and placebo groups.

Airway Resistance↗
PubMed1988

Bioavailability of ambroxol sustained release preparations. Part I: In vitro dissolution studies.

The in vitro dissolution of two ambroxol-HCl containing sustained release preparations (75 mg) and the effect of pH of the dissolution medium on the dissolution rats were investigated. The studies were carried out using the USP XXI paddle method. A new ambroxol HCl sustained release formulation based on a dialyzing membrane for controlled release shows a longer release action as compared to a standard sustained release preparation from commercial source which is based on spheroids constituted by a lipid matrix. The in vitro release rate of the latter product also appears to be more pH dependent.

Ambroxol↗
PubMed1988

Bioavailability of ambroxol sustained release preparations. Part II: Single and multiple oral dose studies in man.

The bioavailability of a new ambroxol sustained release preparation (75 mg) based on a dialyzing membrane for controlled release was studied in healthy volunteers after single and multiple oral dose in comparison with a standard sustained release formulation in a cross-over study under carefully controlled conditions. Plasma concentrations of ambroxol were measured by means of a HPLC method. Based on AUC data both preparations are found to be bioequivalent, but show different plasma concentration profiles. The test preparation showed a more pronounced sustained release profile than the reference preparation (single dose) resulting in significantly higher steady state plasma levels.

Adult↗
PubMed1986

Ambroxol therapy in simple chronic bronchitis: effects on subjective symptoms and ventilatory function.

Ambroxol, a metabolite of bromhexine, was investigated in a double-blind, controlled trial using parallel groups. We studied the effects of 60 mg and 120 mg daily versus placebo in subjects with simple chronic bronchitis. Possible therapeutic effects were evaluated by means of interviews on subjective drug effects and current respiratory symptomatology, patient diary cards, and lung function tests. Ninety-seven subjects entered the study and 92 completed satisfactorily. Comparison with the placebo group at the end of the study showed that significantly more subjects in the 120 mg ambroxol group reported improvement in respiratory symptoms, principally improved expectoration. Subjects in the 120 mg group tended to prefer the treatment period when compared to placebo but the diary cards did not indicate significant changes. Lung function values were mainly normal and did not change during treatment. We conclude that the drug had a symptomatic effect and that further studies in more severely affected patients would be worthwhile.

Adult↗
PubMed1985

Stimulation of lung maturity: investigation of ambroxol in various animal models.

The surfactant or phospholipid lining of the alveolar surface is essential for lung function and airway stability. In premature neonates, the idiopathic respiratory distress syndrome (IRDS) is usually due to a prenatal deficiency in pulmonary surfactant. Experimental and clinical investigations with corticosteroids and other drugs were conducted to study various aspects of lung maturation. The present study of Ambroxol, a new compound with surfactant stimulating properties, was carried out on adult and foetal animals. In adult experimental animals an increase in the activity of Type II pneumocytes was shown by measuring various biochemical parameters. In models of premature animals comparable to clinical IRDS conditions, the antenatal treatment of foetal lambs and rabbits with Ambroxol enhanced lung maturation.

Ambroxol↗
PubMed1978

[Ambroxol, studies of biotransformation in man and determination in biological samples (author's transl)].

15 mg trans-4-[2-amino-3,5-dibromo-benzyl)-amino]-cyclohexanol-hydrochloride (ambroxol, NA 872) was administered i.v. and orally to healthy volunteers. The metabolic pattern in urine and plasma was similar for both routes of administration. Biotransformation reactions are straightforward, yielding two major products of phage I reactions identified as 6,8-dibromo-3-(trans-4-hydroxycyclohexyl)-1,2,3,4-tetrahydro-quinazoline and 3,5-dibromo-anthranilic acid. These metabolites as well as the parent compound are also converted to conjugates, predominantly glucuronides. Quantification of unlabelled ambroxol in biological fluids is achieved by radiochemical derivatisation with 14C-labelled formaldehyde in imitation of the biotransformation.

Administration, Oral↗
PubMed1978

[Therapeutic study on ambroxol in chronic bronchopulmonary diseases (author's transl)].

The clinical activity of trans-4-[(2-amino-3,5-dibromo-benzyl)-amino]-cyclohexanol-hydrochloride (ambroxol, NA 872) as well as its influence on lung function was examined in a total of 63 patients (34 suffering from silicosis, 28 from chronic obstructive bronchitis and 1 from cryptococcosis). Additionally, the content of phospholipids was controlled in the sputum of the patient group. It was shown that the activity of ambroxol was better in the silicosis group than in the bronchitis group. The cause was discussed. Presumably the twofold site of action in the silicosis group (secretolysis and surfactant stimulation) might be the reason for this.

Ambroxol↗
PubMed1978

[Clinical experience with ambroxol syrup (author's transl)].

In an open trial trans-4-[(2-amino-3,5-dibromo-benzyl)-amino]-cyclohexanol hydrochloride (ambroxol, NA 872) in the form of ambroxol syrup was given to non-hospitalised patients suffering from acute and chronic bronchitis. A marked reduction in coughing and dyspnoea as well as an improvement in expectoration was apparent. The maximum effect was reached on the third day of treatment. The effect can be maintained by consistent prolongation of the therapy. There were no side effects.

Administration, Oral↗
PubMed1996

[Clinical evaluation of efficacy and tolerance of oral treatment with ambroxol in patients with chronic bronchitis].

This study was designed to examine the efficacy and tolerability of ambroxol (Ambrosol) on the symptomatology of chronic bronchitis among in- and out-patients. Seventy patients were included in the trial and divided into two random groups. The patients were treated in a double-blind way with either Ambrosol or a placebo for 2 months. The physician and the patient assessed the following points: the feeling general well-being, the symptoms of a cold and of fever, the need for treatment with antibiotics, the amount, viscosity and colour of sputurn, the difficulty in expectoration, the severity of coughing and any changes in breathlessness while at rest. In order to carry out these subjective assessments we used a scoring system. We observed that, breathlessness while at rest and the rate of exacerbation was significantly lower in the Ambrosol group after 2 weeks of therapy. Sputum viscosity, difficulty in expectoration and severity of coughing were reduced in this group after 4 or 8 weeks. Throughout the 2-month period of therapy, the tolerability of ambroxol was good. A total of 4 patients reported side-effects of various degrees of severity. One patient stopped the therapy due to these side-effects (dizziness). There was no significant difference in the number of side-effects between the two groups (Ambrosol vs Placebo).

Administration, Oral↗
PubMed1977

Increased incorporation of fatty acids into phospholipids of lungs and livers of rabbits under the influence of bromhexine and ambroxol.

The incorporation of lauric acid, palmitic acid and oleic acid into phospholipids of lung and liver has been studied in tissue slices of control rabbits and of rabbits treated with bromhexine or ambroxol in doses of 10 mg/kg. A marked increase (up to 200% of the controls) of palmitic acid incorporation into phosphatidylcholine (lecithin) and phosphatidylethanolamine of the lung was found whereas the incorporation rate of palmitic acid into lecithin and phosphatidylethanolamine of the liver displayed no significant change. The incorporation of lauric acid and oleic acid into lung phospholipids was not accelerated. The observed effects were more marked in short time experiments (analysis 2 h after drug injection) than after treatements for 7 days. It is concluded that the phospholipid synthesis is stimulated by the drugs especially in the lungs. This seems to be of particular interest with respect to the surfactant system of the lung and might have some therapeutic relevance.

Ambroxol↗